Biological Activity
Potent and selective tachykinin NK2 receptor antagonist (pKB values are 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors respectively). Active in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data
| M. Wt | 904.08 |
| Formula | C49H61N9O8 |
| Sequence |
AAWFPPX (Modifications: Ala-1 = N-(Bz)Ala, Trp-3 = D-Trp, Pro-5 = D-Pro, X = Nle with C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 141636-65-9 |
| PubChem ID | 5487475 |
| InChI Key | CWEISCOCKRHHOU-UJYVDGJVSA-N |
| Smiles | [H]N([C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N1CCC[C@@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(N)=O)C(=O)C1=CC=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 4 mg/ml in ethanol |
Preparing Stock Solutions
The following data is based on the product molecular weight 904.08. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.11 mL | 5.53 mL | 11.06 mL |
| 5 mM | 0.22 mL | 1.11 mL | 2.21 mL |
| 10 mM | 0.11 mL | 0.55 mL | 1.11 mL |
| 50 mM | 0.02 mL | 0.11 mL | 0.22 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Matuszek et al (1998) An investigation of tachykinin NK2 receptor subtypes in the rat. Eur.J.Pharmacol. 352 103 PMID: 9718274
McElroy et al (1992) Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor. J.Med.Chem. 35 2582 PMID: 1321907
Zagorodnyuk et al (1995) Evidence that tachykinin NK1 and NK2 receptors mediate non-adrenergic non-cholinergic excitation and contraction in the circular muscle of guinea-pig duodenum. Br.J.Pharmacol. 115 237 PMID: 7545517
Keywords: GR 94800, supplier, Potent, selective, NK2, antagonists, Tachykinin, Receptors, Neurokinin, GR94800, GlaxoSmithKline, GSK, NK2, Receptor, NK2, Receptor, Tocris Bioscience
